Advances of AKT Pathway in Human Oncogenesis and as a Target for Anti-Cancer Drug Discovery
Lu-Hai Wang, George Z. Cheng, Sungman Park, Shaokun Shu, Lili He, William Kong, Weizhou Zhang, Zengqiang Yuan and Jin Q. Cheng
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AKT (also known as PKB) plays a central role in a variety of cellular processes including cell growth, motility and survival in both normal and tumor cells. The AKT pathway is also instrumental in epithelial mesenchymal transitions (EMT) and angiogenesis during tumorigenesis. AKT functions as a cardinal nodal point for transducing extracellular (growth factors including insulin, IGF-1 and EGF ) and intracellular (such as mutated/activated receptor tyrosine kinases, PTEN, Ras and Src) signals. It is positively regulated by phosphatidylinositol 3-kinase and inhibited by phosphatase PTEN. Deregulation of the PI3K/PTEN/AKT pathway is one of the most common altered pathways in human malignancy. In the past few years, significant advances have been made in the understanding of AKT signaling in human oncogenesis and the development of small molecule inhibitor of AKT pathway. Here, we will discuss the regulation and function of AKT as well as targeting AKT for anti-cancer drug discovery.
Akt, serine/threonine kinase, oncogene, signal transduction, anti-tumor target, small molecule inhibitor
Department of Microbiology, Mount Sinai School of Medicine, New York, NY 10029, USA.